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• W2069897834 abstract "Ellipticine derivatives have potential as anticancer drugs. Their clinical use has been limited, however, by poor solubility and host toxicity. As N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer−anticancer conjugates are showing promise in early clinical trials, a series of novel HPMA copolymer conjugates have been prepared containing the 6-(3-aminopropyl)-ellipticine derivative (APE, NSC176328). Drug was linked to the polymer via GFLG or GG peptide side chains. To optimize biological behavior, HPMA copolymer-GFLG−APE conjugates with different drug loading (total APE: 2.3−7% w/w; free APE: <0.1% w/w) were synthesized. Conjugation of APE to HPMA copolymers considerably increased its aqueous solubility (>10-fold). HPMA copolymer-GG−APE did not liberate drug in the presence of isolated lysosomal enzymes (tritosomes), but HPMA copolymer-GFLG−APE released APE to a maximum of 60% after 5 h. The rate of drug release was influenced by drug loading; lower loading led to greater release. Whereas free APE (35 μg/mL) caused significant hemolysis (50% after 1 h), HPMA copolymer−APE conjugates were not hemolytic up to 300 μg/mL (APE-equiv). As would be expected from its cellular pharmacokinetics, HPMA copolymer-GFLG−APE was >75 times less cytotoxic than free drug (IC50 ∼ 0.4 μg/mL) against B16F10 melanoma in vitro. However, in vivo when tested in mice bearing s.c. B16F10 melanoma, HPMA copolymer-GFLG−APE (1−10 mg/kg single dose, APE-equiv) given i.p. was somewhat more active (highest T/C value of 143%) than free APE (1 mg/kg) (T/C =127%). HPMA copolymer−APE conjugates warrant further evaluation as potential anticancer agents." @default.
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• W2069897834 date "2001-08-30" @default.
• W2069897834 modified "2023-09-27" @default.
• W2069897834 title "<i>N</i>-(2-Hydroxypropyl)methacrylamide Copolymer−6-(3-Aminopropyl)-ellipticine Conjugates. Synthesis, in Vitro, and Preliminary in Vivo Evaluation" @default.
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• W2069897834 doi "https://doi.org/10.1021/bc0001544" @default.
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